Title:Drug Resistance of Enzalutamide in CRPC
Volume: 19
Issue: 6
Author(s): Xuedong Chen, Jieyang Lu, Liqun Xia and Gonghui Li *
Affiliation:
- Department of Urology, Sir Run-Run Shaw Hospital, College of Medicine, Zhejiang University, Hangzhou, Zhejiang 310006,China
Keywords:
Castration-resistant prostate cancer, enzalutamide, drug resistance, androgen receptor, biomarker, inhibitor.
Abstract: Understanding and targeting the mechanisms of resistance to enzalutamide in castration resistant
prostate cancer.
Background: Enzalutamide (MDV3100, XTANDI) is a second generation androgen receptor inhibitor
that is designed for the treatment of castration-resistant prostate cancer (CRPC) and has prolonged
survival time. The mechanisms of mdv3100 resistance have not yet been clearly clarified and the majority
of treated patients, innate or acquiring resistance invariably arises.
Objective: The purpose of this review is to summarize the main data available on the mechanisms of resistance
to mdv3100. Understanding how the resistance aroused may have clinical implications in underlying
the usefulness of prognostic and predictive biomarkers in daily practice and improving the strategies.
Results: Resistance to MDV3100 could be basically divided into two distinct pathways, either dependent
or independent of the androgen receptor activity. Androgen receptor (AR) axis is sitll the
most important pathway for prostate cancer cells and it is still currently regarded as a critical resistant
mechanism.
Conclusion: Targeting these newly identified signals, especially AR axis, could be potentially overcome
through novel therapeutic agents, synergically improve the ADT in CRPC.
